Powder: -20°C for 3 years | In solvent: -80°C for 1 year
IPA-3 是一种选择性的非 ATP 竞争性 Pak1 抑制剂,IC50 为 2.5 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 178 | 现货 | ||
5 mg | ¥ 377 | 现货 | ||
10 mg | ¥ 568 | 现货 | ||
25 mg | ¥ 1,130 | 现货 | ||
50 mg | ¥ 1,980 | 现货 | ||
100 mg | ¥ 3,570 | 现货 | ||
200 mg | ¥ 5,170 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 392 | 现货 |
产品描述 | IPA-3 is a selective non-ATP competitive Pak1 inhibitor with IC50 of 2.5 μM, no inhibition to group II PAKs (PAKs 4-6). |
靶点活性 | PAK1:2.5 μM |
体外活性 | IPA-3 is a non ATP-competitive, allosteric inhibitor of p21-activated kinase 1 (Pak1). PIR3.5 is the control compound of IPA-3. IPA-3 prevents Cdc42-stimulated Pak1 autophosphorylation on Thr423. IPA-3 also prevents sphingosine-dependent Pak1 autophosphorylation. IPA-3 does not target exposed cysteine residues on Pak1. The disulfide bond of IPA-3 is critical for inhibition of Pak1 and in vitro reduction by the reducing agent dithiothreitol (DTT) abolishes Pak1 inhibition by IPA-3. IPA-3 inhibits activation of Pak1 by diverse activators, but does not inhibit preactivated Pak1. IPA-3 inhibits PDGF-stimulated Pak activation in mouse embryonic fibroblasts. [1] IPA-3 inhibits Pak1 activation in part by binding covalently to the regulatory domain of Pak1. IPA-3 binds Pak1 covalently in a time- and temperature-dependent manner. IPA-3 prevents binding of the Pak1 activator Cdc42. IPA-3 binds directly to the Pak1 autoregulatory domain. IPA-3 reversibly inhibits PMA-induced membrane ruffling in cells. [2] |
激酶实验 | Pak1 (150 nM final) is pre-incubated with MBP (8.3 μM), indicated proteins, and IPA-3 or DMSO in Kinase buffer for 20 minutes at 4°C. Cdc42-GTPγS (3.2 μM) is then added and the reaction is pre-equilibrated 10 minutes at 30°C. Kinase reactions are started by the addition of ATP (to 30 μM) containing [32P]ATP and are incubated 10 min and analyzed by SDS-PAGE and autoradiography. |
细胞实验 | Human primary schwannoma cells are grown on 96 well plates for 2 days. Cells are left untreated or treated with 5 μM IPA-3, 20 μM IPA-3 or 20 μM PIR-3.5 for 24 hours. The MTS-solution is left on the cells for 3 hours, before the absorbance at 490 nm is measured. The experiments are conducted three times and mean and standard error of the mean is calculated with Excel. |
别名 | IPA3, IPA 3 |
分子量 | 350.45 |
分子式 | C20H14O2S2 |
CAS No. | 42521-82-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 7 mg/mL (19.97 mM)
DMSO: 65 mg/mL (185.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.8535 mL | 14.2674 mL | 28.5347 mL | 71.3369 mL |
5 mM | 0.5707 mL | 2.8535 mL | 5.7069 mL | 14.2674 mL | |
10 mM | 0.2853 mL | 1.4267 mL | 2.8535 mL | 7.1337 mL | |
DMSO | 20 mM | 0.1427 mL | 0.7134 mL | 1.4267 mL | 3.5668 mL |
50 mM | 0.0571 mL | 0.2853 mL | 0.5707 mL | 1.4267 mL | |
100 mM | 0.0285 mL | 0.1427 mL | 0.2853 mL | 0.7134 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
IPA-3 42521-82-4 Cytoskeletal Signaling PAK inhibit Inhibitor IPA3 p21 activated kinases IPA 3 inhibitor